What Are the Most Common Dapsone Side Effects?

Si Ze is a drug with molecular formula C9H12N5O4 and molecular weight 255.23. The chemical name of this product is 9- (1,3-dihydroxy-2-propoxymethyl) guanine.

Si Ze

Right!

Size is a

Ganciclovir

Chemical name 9- (1,3-dihydroxy-2-propoxymethyl) -guanine

Molecular formula C9H12N5O4

Molecular weight: 255.23

Specification 0.25g

[Drug alias] Cymevene

[Molecular formula composition] The chemical name of this product is 9- (1,3-dihydroxy-2-propoxymethyl) guanine.

[Specification] Each vial contains 540 mg of lyophilized, white or nearly colorless sodium salt powder, equivalent to 500 mg of propoxyguanosine. 10 mL of water for injection can be formulated into a 50 mg / mL solution with a pH of 11.

[Pharmacology and Toxicology] The intracellular propoxyguanosine is phosphorylated to the monovalent phosphate by the action of deoxyguanosine kinase. It can also be further phosphorylated to the trivalent phosphate by some cell kinases. Cytovirus infected cells are preferentially phosphorylated. The metabolism of propoxyguanosine trivalent phosphate is very slow, and it can still be stored at 60 70% after 18 hours of separation from extracellular fluid. The mechanism of inhibiting viral DNA synthesis is: 1. Competitively inhibits the combination of trivalent phosphate of deoxyguanosine and DNA polymerase; 2. The combination of trivalent nitrate of propoxyguanosine and viral DNA ultimately causes the suspension of DNA extension. It has been found that patients with cytomegalovirus infection treated with this drug can develop acute drug resistance. Propoxyguanosine is a chemically synthesized guanine analog that prevents the replication of herpes virus. Viruses that are sensitive to it include CMV, HSV-1, HSV-2, EBV, VZV. Clinical studies are limited to evaluating the efficacy of patients with cytomegalovirus infection.

[Pharmacokinetics] This medicine is mainly excreted by glomerular filtration. In patients with normal renal function, after continuous injection at a dose of 5 mg / kg body weight for 1 hr, the half-life was 2.9 hr, and the average clearance rate was 3.64 mL / min / kg body weight. At a dose of 5 mg / kg body weight, two injections per day did not cause drug accumulation after 14 days. In patients with renal insufficiency, when the serum creatinine content is <124 mmoL / L, 125-225 mmol / L, and 226-398 mmoL / L, the plasma clearance and half-life of the drug are 3.64 mL / min / kg body weight and 2.9 hr, 2.01 mL / min / kg body weight and 5.3 hr and 1.11 mL / min / kg body weight and 9.7 hr. In patients with severe renal impairment, hemodialysis can reduce drug concentrations by 50%.

[Indications] Prevention and treatment of cytomegalovirus infection in patients with immunodeficiency, such as AIDS patients, tumor patients receiving chemotherapy, and organ transplant patients using immunosuppressants.

[Adverse reactions] Leukocytes and thrombocytopenia are the most common. Anemia, fever, rash, abnormal liver function, edema, infection, and fatigue are rare. Arrhythmia, high / low blood pressure. Abnormal thinking or nightmares, ataxia, coma, dizziness, headache, nervousness, sensory disturbance, psychosis, lethargy, tremor. Nausea, vomiting, diarrhea, gastrointestinal bleeding, abdominal pain. Eosinophils increase and hypoglycemia. Difficulty breathing. Hair loss, itching, hives. Increased hematuria and urea nitrogen. Retinal detachment may occur in AIDS patients with cytomegalovirus-infected retinitis. Infection, pain, and phlebitis can be seen at the injection site.

[Interaction] Probenecid and other drugs that can inhibit renal tubular secretion and reabsorption can reduce the clearance of the drug to the kidney and extend its half-life. The simultaneous use of this drug and drugs that inhibit rapid cell division and replication can produce a synergistic effect. This medicine is used in combination with dapsone, pentanesulfon, flucytosine, vincristine, vinblastine, doxorubicin, amphotericin, trimethoxypyrimidine and some nucleoside drugs, which can increase side effects occur. Most people with AIDS who use this medicine and zidovudine will have severe white blood cell reduction. This drug can be used in combination with imitalen / cilastatin sodium to induce epilepsy.

[Usage and Dosage] Treatment and prevention of cytomegalovirus infection: 5 mg / kg body weight / time, 2 intravenous injections per day, each injection time should exceed 1 hr, and maintain for 14-21 days. Maintenance period: 6 mg / kg body weight / day, 5 days per week or 5 mg / kg body weight / day, 7 days per week, intravenously. When the patient's retinitis develops further, the induction dose needs to be treated again.

The preventive induction amount of cytomegalovirus infection is 5 mg / kg body weight, and it is injected every 12 hr for 7-14 days.

When the patient has renal insufficiency, the induction dose should be adjusted as follows: those with serum creatinine <124 moL / L, the dose remains unchanged; when the blood creatinine is 125-225 moL / L, use 2.5 mg / Kg body weight, twice daily ; When the blood creatinine is 226-398 moL / L, the dose is 2.5 mg / kg body weight, once a day; when the blood creatinine> 398 moL / L, the dose is 1.25 mg / kg body weight, once a day. The optimal maintenance dose is not clear, and the dosage for dialysis patients is 1.25 mg / kg body weight / day. Medication should be taken immediately after the day of dialysis. Symptoms A single intravenous injection of 500 mg / kg to animals can produce vomiting, excessive salivary secretion, bleeding, late purity, abnormal liver function, elevated urea nitrogen, testicular atrophy, and death. Treatment of hemodialysis and increased fluid replacement can reduce drug plasma concentrations. 10 mL of water for injection should be added to each vial, and its preparation solution concentration is 50 mg / mL. Add the drug to 100 mL of intravenous injection solution, and the injection time should exceed 1 hr. 0.9% physiological saline, 5% glucose, sodium lactate injection and Ringer's solution can be compatible with this medicine, and the antibiotic solution containing parabens is not compatible with this medicine. The diluted injection solution should be refrigerated but not frozen, and must be used within 24 hours.

[Precautions] Pregnant and lactating women, those who are allergic to this medicine or acyclovir are contraindicated. Preclinical studies on carcinogenicity, teratogenicity and effects on fertility have found that this drug can cause sperm reduction, mutation, teratogenicity and carcinogenesis, and contraception should be taken within 90 days of stopping treatment. Leukopenia occurs in approximately 10 to 40% of patients treated, so this drug should be used with caution in patients with a history of leukopenia. Thrombocytopenia occurred in 10% of patients treated with this drug (less than 50,000 cells / L), and patients treated with immunosuppressive drugs had a lower decline than patients with AIDS. When the patient's platelet count is less than 100,000 cells / L, the risk of developing thrombocytopenia also increases.

Effects on pregnancy and lactation Animal experiments have found that this drug has teratogenic effects, which cannot be used by pregnant women. This medicine can have adverse effects on the offspring of mammals. It is unknown whether this drug can be secreted into human milk, so it cannot be used in breastfeeding women, and breastfeeding can be resumed after using this drug for 72 hr.

Impact on children The clinical experience of applying to children under 12 years is limited, so children should be used with caution. The adverse effects were reported to be similar to those of adults.

The effect on the elderly should be adjusted according to renal function.